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Koff, A.

Publications and source records attributed to Koff, A..

2 recordsLinked to original sources

CDK4/6 inhibition induces a DNA damage-independent senescence-associated secretory phenotype driven by delayed activation of NF-κB

Cellular senescence consists of regulated cell phenotypes associated with permanent exit from the cell cycle in response to stressors such as genomic instability. The consequences of senescence go beyond individual cells due to the senescence associated secretory phenotype (SASP), which can induce inflammation in neighboring cells. Some cancers respond to CDK4/6 inhibitors (CDK4/6i)--a family of targeted therapies that inhibit proliferation--with a senescence-like phenotype in the absence of DNA damage. We asked how the SASP and the transcriptional regulatory profile triggered by CDK4/6i-driven arrest compares to the canonical NF-{kappa}B-regulated SASP triggered by DNA damage. We profiled the temporal dynamics of transcriptional regulation in response to the CDK4/6i, palbociclib, and the DNA damaging agent, doxorubicin. We found that, although upregulation of NF-{kappa}B driven-SASP genes is shared across both drugs, it is delayed in CDK4/6i. This coincides with slower enhancer activation and epigenetic changes. Interestingly, ATM/ATR inhibition does not affect CDK4/6i-induced NF-{kappa}B nuclear localization, pointing to an alternative mechanism driving NF-{kappa}B activity in the absence of DNA damage. Inhibiting NF-{kappa}B suppresses the expression of shared SASP genes without reversing stable arrest. This points to SASP manipulation as a potential therapeutic strategy, and resolves an ongoing controversy about the nature of cell cycle arrest-driven SASP.

cancer biology↗

Long-term breast cancer response to CDK4/6 inhibition defined by TP53-mediated geroconversion

Inhibition of CDK4/6 kinases has led to improved outcomes in breast cancer. Nevertheless, only a minority of patients experience long-term disease control. Using a clinically-annotated cohort of patients with metastatic HR+ breast cancer, we identified TP53 loss (28.8%) and MDM2 amplification (6.7%) to be associated with lack of long-term disease control. Human breast cancer models revealed that p53 loss did not affect CDK4/6 activity or G1-blockade, but instead promoted drug-insensitive p130 phosphorylation by CDK2. Persistence of phospho-p130 prevented DREAM complex assembly, enabling cell cycle reentry and tumor progression. Inhibitors of CDK2 could overcome p53 loss, leading to geroconversion and manifestation of senescence phenotypes. Complete inhibition of both CDK4/6 and CDK2 kinases appears to be necessary to facilitate long-term response across genomically-diverse HR+ breast cancers.

cancer biology↗